| MonastrolEg5 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.25%
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| Cas No. | 329689-23-8 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | ethyl 6-(3-hydroxyphenyl)-2-mercapto-4-methyl-1,6-dihydropyrimidine-5-carboxylate | ||
| Canonical SMILES | CCOC(C(C1C2=CC(O)=CC=C2)=C(N=C(S)N1)C)=O | ||
| Formula | C14H16N2O3S | M.Wt | 292.35 |
| Solubility | ≥29.2mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 14 μM
Monastrol is a cell-permeable small molecule inhibitor of the mitotic kinesin, Eg5. Like other kinesins, Eg5 can drive the movement of microtubules in vitro.
In vitro: Previous study found that monastrol did not inhibit progression through S and G2 phases of the cell cycle or centrosome duplication. The mitotic arrest due to monastrol was also reversible rapidly. Chromosomes in monastrol-treated cells frequently had both sister kinetochores attached to microtubules extending to the center of the monoaster. Monastrol also inhibited bipolar spindle formation in Xenopus egg extracts, however, monastrol did not prevent the targeting of Eg5 to the monoastral spindles that form [1].
In vivo: Previous study investigated the rat PK and TK of LaSOM 65, a monastrol derivative. Results showed that LaSOM 65 had good bioavailability and linear PK after oral doses. LaSOM 65 distributed consistently in lung and fatty tissues. Other investigated tissues presented smaller penetration ratios. Adverse symptoms were observed only after iv administration, and regressed 3 h after dosing. No statistical differences were found for serum analysis, body weight and relative organ weight, indicating no acute toxicological effects. [2].
Clinical trial: Up to now, LaSOM 65 is still in the preclinical development stage.
References:[1] Kapoor TM,Mayer TU,Coughlin ML,Mitchison TJ. Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5. J Cell Biol.2000 Sep 4;150(5):975-88.[2] Torres BG,Ucha Fde T,Pigatto MC,Azeredo FJ,Haas SE,Dallegrave E,Canto RF,Eifler-Lima VL,Dalla Costa T. Pre-clinical pharmacokinetics and acute toxicological evaluation of a monastrol derivative anticancer candidate LaSOM 65 in rats. Xenobiotica.2014 Mar;44(3):254-63.
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在营养学的范畴里，组氨酸被认为是一种人类必需的氨基酸，主要是儿童。在发育多年之后，人类开始可以自己合成它，在这时便成为非必需氨基酸了。在慢性尿毒症患者的膳食中添加少量的组氨酸，氨基酸结合进入血红蛋白的速度增加，肾原性贫血减轻，所以组氨酸也是尿毒症患者的必需氨酸。 在组氨酸脱羧酶的作用下，组氨酸脱羧形成组胺。组胺具有很强的血管舒张作用，并与多种变态反应及发炎有关。此外，组胺会刺激胃蛋白酶与胃酸。
只有9个氨基酸，分子量1KD左右，想免疫小鼠制备单抗，有没有前辈做过这方面的东西？想了一些方法，但价值不大，请前辈们指教，不甚感激。
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我在看基因方面的文献。基因位点C802T的氨基酸改变H268Y是什么意思啊。求大神指教
